Journal
ARCHIV DER PHARMAZIE
Volume 352, Issue 1, Pages -Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/ardp.201800192
Keywords
1,3-dipolar cycloaddition; anti-malarial activity; anti-proliferative; artemisitene; spiroisoxazoline
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A series of spiroisoxazoline analogues of artemisinin was synthesized by employing 1,3-dipolar cycloaddition between various in situ generated nitrile oxides and artemisitene. All the synthesized compounds were tested for their anti-proliferative and anti-malarial activities. Among the compounds tested, compound 11a was found to be potent against the HCT-15 cancer cell line with IC50 = 4.04 mu M when compared to 5-fluorouracil (IC50 = 35.53 mu M). DNA cell cycle analysis shows that 11a was inhibiting cell proliferation at the G2/M phase. Compound 11b was found to be most active against Plasmodium falciparum with IC50 = 0.1 mu M and also blocked host hemoglobin hydrolysis by the falcipain-3 receptor. It was demonstrated to have better dynamics of parasite killing efficiency than artemisinin. Molecular docking studies revealed that these compounds interacted with falcipain-3 receptor sites.
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